Cholinergics Flashcards Preview

Pharmacology > Cholinergics > Flashcards

Flashcards in Cholinergics Deck (50):
1

Nicotinic Antagonist
Competitive Nn blocker

Use - lowers blood pressure
This drug was introduced in the 50's and there are way better anti-hypertensives

MECAMYLAMINE

2

TACRINE, DONEPZIL, RIVASTIGMINE, GALANTAMINE

Long acting AChE-inhibitors used to treat DEMENTIA

3

BETHANACHOL

Half-life - long, not a substrate for acetylcholinesterase

Use - Nonobstructive GI Disorders or URINARY RETENTION

Stimulate GI motility and bladder emptying

4

d-Tubocurarine

Muscle relaxant
Active component in curare, hypotension
Rarely used due to tendency to release histamine and cause bronchospasm
Some cross reactivity with Nn

5

CARBACHOL

Half-life - long, not a substrate for acetylcholinesterase

Pupillary constriction
Use - limited, because nicotinic activity stimulates all autonomic ganglia

Some application in treating glaucoma

6

More selective for M1, which lessens side effects
Less tendency for dry mouth/blurred vision
Peptic Ulcer Disease - suppresses acid secretion via action on parietal cells

PIRENZIPINE

7

TIOTROPIUM

Bronchodilation

Supposedly more bronchoselective than ipratropium
Has less affinity for M2 receptors (doesn't cause cardiac side effects)
Increase exercise tolerance

8

Spasmolytic
Stimulates presynaptic GABA-B receptors, suppressing excitatory transmissions

BACLOFEN

9

Similar to neostigmine but with a longer duration
MYASTHENIA GRAVIS — primary drug

PYRIDOSTIMINE

10

Inhibits calcium release from sarcoplasmic reticulum
Treat malignant hypertherima

DANTROLENE

11

Muscle relaxant
Active component in curare, hypotension
Rarely used due to tendency to release histamine and cause bronchospasm
Some cross reactivity with Nn

d-Tubocurarine

12

Chronic Asthma/COPD - induces bronchodilation but does not inhibit ciliary motility
Note for acute asthma attacks (beta-2 agonists are much better)
Rhinorrhea — stops runny nose

IPRATROPIUM

13

MECAMYLAMINE

Nicotinic Antagonist
Competitive Nn blocker

Use - lowers blood pressure
This drug was introduced in the 50's and there are way better anti-hypertensives

14

ATROPINE

M1, M2, and M3 receptors
Eyes - causes MYDRIASIS & CYCLOPLEGIA
Promotes BRONCHODILATION and reduces secretions

Initial bradycardia, but in general causes TACHYCARDIA
TREAT AV-blocks and post-MI bradycardia

GI - antispasmodic, can be used to treat IBS

Use for OVERACTIVE BLADDER

Anti-AchE poisoning

15

BACLOFEN

Spasmolytic
Stimulates presynaptic GABA-B receptors, suppressing excitatory transmissions

16

PYRIDOSTIMINE

Similar to neostigmine but with a longer duration
MYASTHENIA GRAVIS — primary drug

17

TOLTERODINE, OXYBUTYNIN, DARIFENACIN, SOLIFENACIN

Slightly more selective for the M3 receptors
Used to treat OVERACTIVE BLADDER and incontinence
Neurologic problems

18

SUCCINYLCHOLINE

Depolarizing blocker
Hyperkalemia
Myalgia
Ganglionic Stimulation
Malignant Hyperthermia

19

Eyes - causes MYDRIASIS & CYCLOPLEGIA
Promotes BRONCHODILATION and reduces secretions

Initial bradycardia, but in general causes TACHYCARDIA
TREAT AV-blocks and post-MI bradycardia

GI - antispasmodic, can be used to treat IBS

Use for OVERACTIVE BLADDER

Anti-AchE poisoning

ATROPINE

20

Prophylactic for MOTION SICKNESS
Can be used as a patch

SCOPOLAMINE

21

Depolarizing blocker
Hyperkalemia
Myalgia
Ganglionic Stimulation
Malignant Hyperthermia

SUCCINYLCHOLINE

22

PIRENZIPINE

More selective for M1, which lessens side effects
Less tendency for dry mouth/blurred vision
Peptic Ulcer Disease - suppresses acid secretion via action on parietal cells

23

Partial nicotinic agonist that reduces nicotine craving
Causes nightmares

VARENCICLINE

24

Covalently bind and inactivate AChE, undergo aging (irreversible)

SLUDGEM symptoms - Bradycardic, Excessive Tearing, Can’t breathe

Parathion, Malathion, Echothiophate

25

Use — DIAGNOSIS of myasthenia gravis via injection
Cholinergic Crisis (Tensilon Test) - identify if they are OVER or UNDER treated

EDROPHONIUM

26

IPRATROPIUM

Chronic Asthma/COPD - induces bronchodilation but does not inhibit ciliary motility
Note for acute asthma attacks (beta-2 agonists are much better)
Rhinorrhea — stops runny nose

27

Anti-Cholinergic Toxicity

Hot dry skin, Dry mouth, Dry eyes
Mydriasis and Cyclopegia —> Blurred vision (Blind as a bat)

Narrowing of anterior chamber and diminished outflow of aqueous humor

Sedation, Agitation, Hallucination, Coma (Mad as a Hatter)

28

PILOCARPINE

Half-life - long, not a substrate for acetylcholinesterase

Glaucoma - contracts ciliary muscle and increases outflow of aqueous humor

Xerostomia - stimulates salivary glands, useful in Sjorgen's syndrome

Can cause Diaphoresis

29

GI atony - used in cases of post-operative paralysis of the GI tract
GU atony - used in post-operative dysuria
Glaucoma - miosis, lowers IOP
Myasthenia Gravis - most common treatment in the US, increases Ach concentration @ NMJ
NM blockade reversal - reverses paralysis from competitive NM blockade agents (eg Curare and related drugs)

NEOSTIGMINE

30

Act on GABA receptors in the CNS

DIAZEPAM

31

Long acting AChE-inhibitors used to treat DEMENTIA

TACRINE, DONEPZIL, RIVASTIGMINE, GALANTAMINE

32

Half-life - long, not a substrate for acetylcholinesterase

Use - Nonobstructive GI Disorders or URINARY RETENTION

Stimulate GI motility and bladder emptying

BETHANACHOL

33

Slightly more selective for the M3 receptors
Used to treat OVERACTIVE BLADDER and incontinence
Neurologic problems

TOLTERODINE, OXYBUTYNIN, DARIFENACIN, SOLIFENACIN

34

METHACHOLINE

No effect in normal patients, but will provoke airway constriction in asthmatics

Used to diagnose bronchial hyperreactivity (asthma) WHEEZING

35

SCOPOLAMINE

Prophylactic for MOTION SICKNESS
Can be used as a patch

36

No effect in normal patients, but will provoke airway constriction in asthmatics

Used to diagnose bronchial hyperreactivity (asthma) WHEEZING

METHACHOLINE

37

EDROPHONIUM

Use — DIAGNOSIS of myasthenia gravis via injection
Cholinergic Crisis (Tensilon Test) - identify if they are OVER or UNDER treated

38

Parathion, Malathion, Echothiophate

Organophosphates
Covalently bind and inactivate AChE, undergo aging (irreversible)

SLUDGEM symptoms - Bradycardic, Excessive Tearing, Can’t breathe

Tx: Pralidoximine, Atropine

39

Half-life - long, not a substrate for acetylcholinesterase

Glaucoma - contracts ciliary muscle and increases outflow of aqueous humor

Xerostomia - stimulates salivary glands, useful in Sjorgen's syndrome

Can cause Diaphoresis

PILOCARPINE

40

Bronchodilation

Has less affinity for M2 receptors (doesn't cause cardiac side effects)
Increase exercise tolerance

TIOTROPIUM

41

VARENCICLINE ("Chantix")

Partial nicotinic agonist that reduces nicotine craving
Causes nightmares

1-800-VERY CLEAN

42

Sometimes used in ophthalmic surgery to constrict pupil (Miochol)

Acetylcholine

43

Acetylcholine

Half-life - very short, rapidly metabolized by acetylcholinesterase

Use - Limited clinical use due to potential side effects, sometimes used in ophthalmic surgery to constrict pupil (Miochol)

44

NEOSTIGMINE

GI atony - used in cases of post-operative paralysis of the GI tract
GU atony - used in post-operative dysuria
Glaucoma - miosis, lowers IOP
Myasthenia Gravis - most common treatment in the US, increases Ach concentration @ NMJ
NM blockade reversal - reverses paralysis from competitive NM blockade agents (eg Curare and related drugs)

45

DIAZEPAM

Spasmolytic
Benzodiazepines act on GABA receptors in the CNS

46

Rocuronium

Muscle relaxant for surgery
Nm selective, no CV side effects

47

Muscle relaxant for surgery
Nm selective, no CV side effects

Rocuronium

48

DANTROLENE

Inhibits calcium release from sarcoplasmic reticulum
Treat malignant hyperthermia

49

Half-life - long, not a substrate for acetylcholinesterase

Pupillary constriction
Use - limited, because nicotinic activity stimulates all autonomic ganglia

Some application in treating glaucoma

CARBACHOL

50

Hot dry skin, Dry mouth, Dry eyes
Mydriasis and Cyclopegia —> Blurred vision (Blind as a bat)

Narrowing of anterior chamber and diminished outflow of aqueous humor

Sedation, Agitation, Hallucination, Coma (Mad as a Hatter)

Anti-Cholinergic Toxicity